TW201144302A - 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds - Google Patents
2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compoundsInfo
- Publication number
- TW201144302A TW201144302A TW100115662A TW100115662A TW201144302A TW 201144302 A TW201144302 A TW 201144302A TW 100115662 A TW100115662 A TW 100115662A TW 100115662 A TW100115662 A TW 100115662A TW 201144302 A TW201144302 A TW 201144302A
- Authority
- TW
- Taiwan
- Prior art keywords
- oxazepin
- tetrahydro
- ylamine
- compounds
- diabetes
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10162340 | 2010-05-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
TW201144302A true TW201144302A (en) | 2011-12-16 |
Family
ID=44168838
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
TW100115662A TW201144302A (en) | 2010-05-07 | 2011-05-04 | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
Country Status (14)
Country | Link |
---|---|
US (2) | US8673894B2 (en) |
EP (1) | EP2566855B1 (en) |
JP (1) | JP5823503B2 (en) |
KR (1) | KR20130100241A (en) |
CN (1) | CN102958922B (en) |
AR (1) | AR081369A1 (en) |
BR (1) | BR112012028519A2 (en) |
CA (1) | CA2797622A1 (en) |
ES (1) | ES2481409T3 (en) |
HK (1) | HK1179617A1 (en) |
MX (1) | MX2012012952A (en) |
RU (1) | RU2570796C2 (en) |
TW (1) | TW201144302A (en) |
WO (1) | WO2011138293A1 (en) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2572263T3 (en) | 2005-10-25 | 2016-05-31 | Shionogi & Co | Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors |
ES2476605T3 (en) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Aminohydrotiazine derivatives substituted with cyclic groups |
JP5383483B2 (en) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | Pharmaceutical composition for the treatment of Alzheimer's disease |
CN102119161B (en) | 2008-06-13 | 2015-07-08 | 盐野义制药株式会社 | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-aminopyridin-4-one and 2-aminopyridine derivative both having bace1-inhibiting activity |
AR077328A1 (en) * | 2009-07-24 | 2011-08-17 | Novartis Ag | DERIVATIVES OF OXAZINE AND ITS USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS |
UA108363C2 (en) | 2009-10-08 | 2015-04-27 | IMINOTIADIASIADIOXIDE OXIDES AS BACE INHIBITORS, COMPOSITIONS THEREOF AND THEIR APPLICATIONS | |
UA110467C2 (en) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Oxazine derivatives |
WO2012057248A1 (en) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | Naphthyridine derivative |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
PL2663561T3 (en) | 2011-01-13 | 2016-10-31 | Novel heterocyclic derivatives and their use in the treatment of neurological disorders | |
CA2824493A1 (en) * | 2011-01-13 | 2012-07-19 | Novartis Ag | Bace-2 inhibitors for the treatment of metabolic disorders |
US9242943B2 (en) * | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
US8815841B2 (en) * | 2011-02-18 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
US8748418B2 (en) * | 2011-03-18 | 2014-06-10 | Hoffmann-La Roche Inc. | 1,4-oxazepines as BACE1 and/or BACE2 inhibitors |
US8877744B2 (en) * | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2697210B1 (en) | 2011-04-13 | 2017-03-01 | Merck Sharp & Dohme Corp. | 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions, and their use |
TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
US8927535B2 (en) * | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
WO2013028670A1 (en) | 2011-08-22 | 2013-02-28 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
IN2014DN03206A (en) | 2011-10-13 | 2015-05-22 | Novartis Ag | |
US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
CN104245680B (en) | 2012-04-27 | 2016-11-23 | 卫材R&D管理有限公司 | For producing the method for 5-(difluoromethyl) pyrazine-2-formic acid and producing intermediate |
US9556135B2 (en) | 2012-10-12 | 2017-01-31 | Amgen, Inc. | Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
JP2016504998A (en) | 2012-12-20 | 2016-02-18 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | C5, C6 oxacyclic fused iminothiazine dioxide compounds, compositions and their use as BACE inhibitors |
CA2903215C (en) * | 2013-03-08 | 2021-07-20 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
US9745324B2 (en) | 2013-12-18 | 2017-08-29 | Merck Sharp & Dohme Corp. | Iminothiadiazepane dioxide compounds as BACE inhibitors, compositions, and their use |
JP6674960B2 (en) | 2015-03-20 | 2020-04-01 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | BACE1 inhibitor |
TW201726651A (en) | 2015-09-23 | 2017-08-01 | 健生藥品公司 | 2,3,4,5-tetrahydropyridin-6-amine derivatives |
CN108774195A (en) * | 2018-05-18 | 2018-11-09 | 河南福萌商贸有限公司 | A kind of synthetic method of thiazole carboxylic acid's class chemical intermediate intermediate product |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4268509A (en) | 1978-07-10 | 1981-05-19 | Fujisawa Pharmaceutical Co., Ltd. | New cephem compounds and processes for preparation thereof |
RU2170732C2 (en) * | 1993-04-19 | 2001-07-20 | Такеда Кемикал Индастриз, Лтд. | Derivatives of 4,1-benzoxazepine |
NZ544200A (en) | 2003-07-14 | 2009-07-31 | Arena Pharm Inc | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
ES2572263T3 (en) * | 2005-10-25 | 2016-05-31 | Shionogi & Co | Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors |
ES2476605T3 (en) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Aminohydrotiazine derivatives substituted with cyclic groups |
WO2009081789A1 (en) | 2007-12-26 | 2009-07-02 | Banyu Pharmaceutical Co., Ltd. | Sulfonyl substituted 6-membered ring derivative |
US8158620B2 (en) | 2008-01-18 | 2012-04-17 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivatives |
CN102119161B (en) | 2008-06-13 | 2015-07-08 | 盐野义制药株式会社 | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
AR077328A1 (en) * | 2009-07-24 | 2011-08-17 | Novartis Ag | DERIVATIVES OF OXAZINE AND ITS USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS |
-
2011
- 2011-04-28 US US13/096,059 patent/US8673894B2/en not_active Expired - Fee Related
- 2011-05-03 MX MX2012012952A patent/MX2012012952A/en not_active Application Discontinuation
- 2011-05-03 CA CA2797622A patent/CA2797622A1/en not_active Abandoned
- 2011-05-03 RU RU2012148818/04A patent/RU2570796C2/en not_active IP Right Cessation
- 2011-05-03 KR KR1020127031991A patent/KR20130100241A/en not_active Application Discontinuation
- 2011-05-03 ES ES11720065.9T patent/ES2481409T3/en active Active
- 2011-05-03 EP EP11720065.9A patent/EP2566855B1/en not_active Not-in-force
- 2011-05-03 JP JP2013509501A patent/JP5823503B2/en not_active Expired - Fee Related
- 2011-05-03 BR BR112012028519A patent/BR112012028519A2/en not_active IP Right Cessation
- 2011-05-03 CN CN201180023097.2A patent/CN102958922B/en not_active Expired - Fee Related
- 2011-05-03 WO PCT/EP2011/056990 patent/WO2011138293A1/en active Application Filing
- 2011-05-04 TW TW100115662A patent/TW201144302A/en unknown
- 2011-05-05 AR ARP110101549A patent/AR081369A1/en not_active Application Discontinuation
-
2013
- 2013-06-07 HK HK13106766.4A patent/HK1179617A1/en not_active IP Right Cessation
- 2013-10-22 US US14/059,910 patent/US20140045820A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
CN102958922A (en) | 2013-03-06 |
US20110312937A1 (en) | 2011-12-22 |
US20140045820A1 (en) | 2014-02-13 |
KR20130100241A (en) | 2013-09-10 |
RU2570796C2 (en) | 2015-12-10 |
EP2566855A1 (en) | 2013-03-13 |
HK1179617A1 (en) | 2013-10-04 |
WO2011138293A1 (en) | 2011-11-10 |
EP2566855B1 (en) | 2014-05-21 |
JP5823503B2 (en) | 2015-11-25 |
US8673894B2 (en) | 2014-03-18 |
AR081369A1 (en) | 2012-08-29 |
JP2013525506A (en) | 2013-06-20 |
ES2481409T3 (en) | 2014-07-30 |
MX2012012952A (en) | 2012-12-17 |
CA2797622A1 (en) | 2011-11-10 |
BR112012028519A2 (en) | 2016-07-19 |
RU2012148818A (en) | 2014-06-20 |
CN102958922B (en) | 2015-09-30 |
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